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1. 发明授权

US07750156B2 Method of producing aminophenol compounds 失效
标题翻译：制备氨基苯酚化合物的方法
公开(公告)号：US07750156B2
公开(公告)日：2010-07-06
申请号：US10593968
申请日：2005-03-25
申请人： Hiroshi Kiyokawa , Shinji Aki
发明人： Hiroshi Kiyokawa , Shinji Aki
IPC分类号： C07D241/04 , C07D401/00 , C07D211/40
CPC分类号： C07D295/096 , C07C213/02 , C07C215/76 , C07C215/82
摘要： The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.
摘要翻译：本发明提供了一种工业上有利的方法，通过简单和容易的方法以高产率和高纯度制备由式（1）表示的氨基苯酚化合物。本发明提供一种由式（1）表示的氨基苯酚化合物的制造方法：（其中R 1和R 2可以相同或不同，为氢原子，取代或未取代的低级烷基等 ; R 1和R 2与相邻的氮原子一起可以与有或没有其它插入的杂原子形成5-或6-元杂环;该杂环可以被1至3个选自羟基，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳氧基等;式（1）中的羟基在2-或4-位被氨基取代，苯环），其包括使式（2）表示的环己二酮化合物与式（3）表示的胺化合物（其中R 1和R 2如上所定义）在中性或碱性下反应 c条件。

2. 发明授权

US07399864B2 Process for producing carbostyril derivatives 有权
标题翻译：喹诺酮衍生物的制备方法
公开(公告)号：US07399864B2
公开(公告)日：2008-07-15
申请号：US10208738
申请日：2002-08-01
申请人： Shinji Aki , Muneaki Kurimura , Takao Nishi , Junichi Minamikawa , Michiaki Tominaga
发明人： Shinji Aki , Muneaki Kurimura , Takao Nishi , Junichi Minamikawa , Michiaki Tominaga
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , A61K31/4709
摘要： The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.
摘要翻译：本发明提供了以高产率和高纯度制备喹诺酮衍生物（I）的方法，已知其可用作药物如抗血栓形成剂，脑循环改进剂，抗炎剂，抗溃疡剂等。喹诺酮衍生物（I）可以通过在相转移催化剂存在下使喹诺酮衍生物（II）与四唑衍生物（III）反应来制备。

3. 发明授权

US4880806A 1-Cyclopropyl-6-fl uoro-7-piperazinyl-1,4-Dihydro-4-oxo-quinoline-3-carboxylic acid derivatives 失效
标题翻译： 1-环丙基-6-氟-7-哌嗪基-1,4-二氢-4-氧代 - 喹啉-3-羧酸衍生物
公开(公告)号：US4880806A
公开(公告)日：1989-11-14
申请号：US76890
申请日：1987-07-23
申请人： Hiraki Ueda , Hisashi Miyamoto , Shinji Aki , Tatsuya Otsuka
发明人： Hiraki Ueda , Hisashi Miyamoto , Shinji Aki , Tatsuya Otsuka
IPC分类号： C07D215/56 , C07D401/04 , C07D405/12 , C07D487/04
CPC分类号： C07D215/56 , C07D401/04 , C07D405/12 , C07D487/04
摘要： Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.2 is a heterocyclic group: ##STR2## in which R.sup.A is H, C.sub.1 -C.sub.6 alkyl or phenyl (C.sub.1 -C.sub.6) alkyl, R.sup.B is 2-oxo-1,3-dioxolenemethyl substituted by C.sub.1 -C.sub.6 alkyl, or C.sub.3 -C.sub.8 cycloalkyl, R.sup.C is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, or phenyl(C.sub.1 -C.sub.6)alkyl, R.sup.D is H or C.sub.1 -C.sub.6 alkyl, R.sup.G is C.sub.1 -C.sub.6 alkyl, and R.sup.H is C.sub.1 -C.sub.6 alkyl, phenyl(C.sub.1 -C.sub.6)alkyl, or C.sub.1 C.sub.6 alkanoyl, and R.sup.3 is C.sub.1 -C.sub.6 alkyl, or R.sup.3 is C.sub.1 -C.sub.6 alkyl having 1 to 3 substituents selected from OH, C.sub.1 -C.sub.6 alkoxy and halogen when R.sup.2 is ##STR3## or a salt thereof, said compounds having excellent antimicrobial activity and being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
摘要翻译：新颖的下式的4-氧代喹啉-3-羧酸化合物：其中R 2是杂环基：其中RA是H，C 1 -C 6烷基或苯基（C 1 -C 6） C6）烷基，RB是被C1-C6烷基或C3-C8环烷基取代的2-氧代-1,3-二氧杂环戊烯甲基，RC是H，C1-C6烷基，C1-C6烷氧基羰基或苯基（C1-C6）烷基，RD为H或C1-C6烷基，RG为C1-C6烷基，RH为C1-C6烷基，苯基（C1-C6）烷基或C1C6烷酰基，R3为C1-C6烷基，R3为C1- 当R2为1或3个选自OH，C1-C6烷氧基和卤素的取代基时，具有1至3个取代基的C6烷基或其盐，所述具有优异抗微生物活性并可用作抗微生物剂的化合物和含有所述化合物的药物组合物活性成分。

4. 发明授权

US08598358B2 Synthetic intermediate of oxazole compound and method for producing the same 有权
标题翻译：恶唑化合物的合成中间体及其制造方法
公开(公告)号：US08598358B2
公开(公告)日：2013-12-03
申请号：US13574546
申请日：2011-01-28
申请人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
发明人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
IPC分类号： C07D211/46 , C07D405/12 , C07D498/04
CPC分类号： C07D211/46 , C07D405/12 , C07D498/04
摘要： An object of the present invention is to provide a method for producing an oxazole compound in a high yield.The object can be achieved by a compound represented by Formula (11): wherein R1 is a hydrogen atom or lower-alkyl group; R2 is a 1-piperidyl group substituted at the 4-position with a substituent selected from (A1a) a phenoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1b) a phenoxy-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkyl groups, (A1c) a phenyl-substituted lower-alkoxy lower-alkyl group substituted on the phenyl moiety with halogen, (A1d) a phenyl-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1e) an amino group substituted with a phenyl group substituted with one or more halogen-substituted lower-alkoxy groups, and a lower-alkyl group, and (A1f) a phenyl-substituted lower-alkoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups; n is an integer from 1 to 6; and X3 is an organic sulfonyloxy group.
摘要翻译：本发明的目的是提供以高产率制备恶唑化合物的方法。该目的可以通过式（11）表示的化合物来实现：其中R1是氢原子或低级烷基; R2是在4-位被取代基取代的1-哌啶基，该取代基选自（A1a）苯基部分被一个或多个卤素取代的低级烷氧基取代的苯氧基，（A1b）苯氧基取代的低级烷氧基，在苯基部分上被一个或多个卤素取代的低级烷基取代的烷基（A1c）在苯基部分被卤素取代的苯基取代的低级烷氧基低级烷基，（A1d）苯基取代的低级烷基，在苯基部分被一个或多个卤素取代的低级烷氧基取代的烷基，（A1e）被被一个或多个卤素取代的低级烷氧基取代的苯基取代的氨基和低级烷基，和（A1f）在苯基部分上被一个或多个卤素取代的低级烷氧基取代的苯基取代的低级烷氧基; n是1至6的整数; X3是有机磺酰氧基。

5. 发明授权

US08222276B2 Amine salt of carbostyril derivative 有权
标题翻译：喹诺酮衍生物的胺盐
公开(公告)号：US08222276B2
公开(公告)日：2012-07-17
申请号：US12662610
申请日：2010-04-26
申请人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-ichiro Sumida
发明人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-ichiro Sumida
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D215/227
摘要： The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.
摘要翻译：本发明提供由式（1）表示的喹诺酮衍生物形成的喹诺酮衍生物的胺盐[其中R是卤素原子; 侧链的取代位置是喹诺酮骨架中的3-或4-位; 并且喹诺酮骨架的3-和4-位之间的键合是单键或双键]和胺; 本发明由于具有优异的水溶性和优异的药理作用而用作治疗各种疾病的药物，特别是作为水性制剂。

6. 发明申请

US20100210684A1 Amine salt of carbostyril derivative 有权
公开(公告)号：US20100210684A1
公开(公告)日：2010-08-19
申请号：US12662610
申请日：2010-04-26
申请人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-Ichiro Sumida
发明人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-Ichiro Sumida
IPC分类号： A61K31/47 , C07D215/227
CPC分类号： C07D215/227
摘要： The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.

7. 发明申请

US20070155787A1 Amine salt of carbostyril derivative 失效
标题翻译：喹诺酮衍生物的胺盐
公开(公告)号：US20070155787A1
公开(公告)日：2007-07-05
申请号：US10586453
申请日：2005-01-20
申请人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-ichiro Sumida
发明人： Yoshihiro Nishioka , Shinji Aki , Shigekazu Fujita , Yoshinao Onishi , Shun-ichiro Sumida
IPC分类号： A61K31/4704 , C07D215/22
CPC分类号： C07D215/227
摘要： The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double H bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.
摘要翻译：本发明提供由式（1）表示的喹诺酮衍生物形成的喹诺酮衍生物的胺盐[其中R是卤素原子; 侧链的取代位置是喹诺酮骨架中的3-或4-位; 并且喹诺酮骨架的3-和4-位之间的键合是单键或双H键]和胺; 本发明由于具有优异的水溶性和优异的药理作用而用作治疗各种疾病的药物，特别是作为水性制剂。

8. 发明申请

US20060100437A1 Process for producing carbostyril derivatives 审中-公开
公开(公告)号：US20060100437A1
公开(公告)日：2006-05-11
申请号：US11318104
申请日：2005-12-23
申请人： Shinji Aki , Muneaki Kurimura , Takao Nishi , Junichi Minamikawa , Michiaki Tominaga , Norihiro Fukuyama , Akihiro Yamamoto
发明人： Shinji Aki , Muneaki Kurimura , Takao Nishi , Junichi Minamikawa , Michiaki Tominaga , Norihiro Fukuyama , Akihiro Yamamoto
IPC分类号： C07D403/02
CPC分类号： C07D401/12
摘要： The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.

9. 发明授权

US4874764A Benzoheterocyclic compounds 失效
标题翻译：苯并杂环化合物
公开(公告)号：US4874764A
公开(公告)日：1989-10-17
申请号：US63401
申请日：1987-06-18
申请人： Hiraki Ueda , Hisashi Miyamoto , Shinji Aki , Tatsuya Otsuka
发明人： Hiraki Ueda , Hisashi Miyamoto , Shinji Aki , Tatsuya Otsuka
IPC分类号： C07D215/56 , C07D401/04 , C07D405/12 , C07D487/04
CPC分类号： C07D215/56 , C07D401/04 , C07D405/12 , C07D487/04
摘要： Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl and R.sup.F is C.sub.1 -C.sub.6 alkyl, and a pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
摘要翻译：具有下式的新颖的4-氧代喹啉-3-羧酸化合物：其中R 3是C 1 -C 6烷基且RF是C 1 -C 6烷基，其药学上可接受的盐，所述化合物具有优异的抗微生物活性，因此可用作抗微生物剂，以及含有所述化合物作为活性成分的药物组合物。

10. 发明申请

US20120302757A1 SYNTHETIC INTERMEDIATE OF OXAZOLE COMPOUND AND METHOD FOR PRODUCING THE SAME 有权
标题翻译：奥扎唑化合物的合成中间体及其制备方法
公开(公告)号：US20120302757A1
公开(公告)日：2012-11-29
申请号：US13574546
申请日：2011-01-28
申请人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
发明人： Akihiro Yamamoto , Koichi Shinhama , Nobuhisa Fujita , Shinji Aki , Shin Ogasawara , Naoto Utsumi
IPC分类号： C07D211/22 , C07D498/04 , C07D211/58 , C07D405/12
CPC分类号： C07D211/46 , C07D405/12 , C07D498/04
摘要： An object of the present invention is to provide a method for producing an oxazole compound in a high yield.The object can be achieved by a compound represented by Formula (11): wherein R1 is a hydrogen atom or lower-alkyl group; R2 is a 1-piperidyl group substituted at the 4-position with a substituent selected from (A1a) a phenoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1b) a phenoxy-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkyl groups, (A1c) a phenyl-substituted lower-alkoxy lower-alkyl group substituted on the phenyl moiety with halogen, (A1d) a phenyl-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1e) an amino group substituted with a phenyl group substituted with one or more halogen-substituted lower-alkoxy groups, and a lower-alkyl group, and (A1f) a phenyl-substituted lower-alkoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups; n is an integer from 1 to 6; and X3 is an organic sulfonyloxy group.
摘要翻译：本发明的目的是提供以高产率制备恶唑化合物的方法。该目的可以通过式（11）表示的化合物来实现：其中R1是氢原子或低级烷基; R2是在4-位被取代基取代的1-哌啶基，该取代基选自（A1a）苯基部分被一个或多个卤素取代的低级烷氧基取代的苯氧基，（A1b）苯氧基取代的低级烷氧基，在苯基部分上被一个或多个卤素取代的低级烷基取代的烷基（A1c）在苯基部分被卤素取代的苯基取代的低级烷氧基低级烷基，（A1d）苯基取代的低级烷基，在苯基部分被一个或多个卤素取代的低级烷氧基取代的烷基，（A1e）被被一个或多个卤素取代的低级烷氧基取代的苯基取代的氨基和低级烷基，和（A1f）在苯基部分上被一个或多个卤素取代的低级烷氧基取代的苯基取代的低级烷氧基; n是1至6的整数; X3是有机磺酰氧基。

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